Heterocyclic Building Blocks-piperazine

112984-60-8, 6-Fluoro-1-methyl-4-oxo-7-(piperazin-1-yl)-1,4-dihydro-[1,3]thiazeto[3,2-a]quinoline-3-carboxylic acid is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Synthesis of e-Ffuoro–methyl-T-l^ l-Cl-methyl-S-nitro-iniidazol- l-y)-ethyl]-piperazm-l -yl}-4-oxo-4H-2-th5a-8b-aza-cyclobiita[a]naphihafene- 3-carboxyfic acid (119): To a stirred solution of 6-Fluoro- l -methyl-4-oxo-7- piperazin- 1 -yl-4H-2-ihia-8 -aza-cyclobuta[a]naphihaiene-3-earboxyiic acid, (II) (5. 1 6g. 14,76 mmol ) in dimethylforrnarnide ( 1 00ml) was added potassium carbonate (2.03g, 14.76 mmol) followed by addition of compound (I) (2g, 7.2 mmol) and the reaction mixture was heated at 90 C for 16h. The reaction mixture was di luted with ethyl acetate, washed twice with water and finally dried over sodium sulphate to obtain the crude mass. The crude was purified by flash column chromatography while eluting with 4-5% methanol/dichlorornethane mixture to obtain the pure compound ( 1 19) with 20% isolated yield. FontWeight=”Bold” FontSize=”10″ H-NMR (400 MHz, CDCI3) 5ppm: 2.12 (3H, d, J = 6.4 Hz, CH3), 2.52 (3H, s, CH3), 2.64 (4H, m, 2 xCH2), 2.72(2H, t, J = 6 Hz, CH2), 3.1 1 -3. 18 (4H, m, 2 x CH2), 4.43-4.49 (2H, m, CH2N). 5.8-5.9 ( 1 H, q, J,= 6.4Hz, J2 = 1 2.8Hz, CHSN), 6.3 (3 H, d, J = 6.8Hz, Ar- H), 7.92 (1 H, s, Ar-H), 7.95 ( 1 H, s, Ar-H). ESf-MS (m/z): 503 (M+H)

112984-60-8, The synthetic route of 112984-60-8 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; VYOME BIOSCIENCES PVT. LTD.; SENGUPTA, Shiladitya; CHAWRAI, Suresh Rameshlal; GHOSH, Shamik; GHOSH, Sumana; JAIN, Nilu; SADHASIVAM, Suresh; BUCHTA, Richard; BHATTACHARYYA, Anamika; WO2015/114666; (2015); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.128102-16-9,(R)-4-Benzyl 1-Boc-2-methylpiperazine-4-carboxylate,as a common compound, the synthetic route is as follows.

A solution of 4-benzyl 1-tert-butyl 2-methylpiperazine-1,4-dicarboxylate (4.8 g, 14.4 mmol) in methanol (25 mL) was added 480 mg of 10% Pd/C and stirred at room temperature under hydrogen overnight. Filtered and concentrated to give the title product (2.8 g, yield 97%) as colorless oil. 1H-NMR (400 MHz, CDCl3) delta (ppm): 1.21 (d, J=6.8 Hz, 3H), 1.46 (s, 9H), 2.64-2.70 (m, 1H), 2.74-2.78 (m, 1H), 2.88-3.01 (m, 3H), 3.78 (d, J=12.4 Hz, 1H), 4.16 (m, 1H); LC-MS (ESI) m/z: 201 (M+1)+, 128102-16-9

The synthetic route of 128102-16-9 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; LEAD THERAPEUTICS, INC.; US2010/35883; (2010); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.13889-98-0,1-Acetylpiperazine,as a common compound, the synthetic route is as follows.

In a three neck flask, under inert atmosphere (N2), is added 7.19g (27.2mmol) ofD in 150ml of DCM. The mixture is cooled to 0C. Then 5.75g (30mmol) of EDCI, 4.05g (30mmol) of HOBt and 3.85g (30mmol) of acetylpiperazine are added in this order. The temperature of 0C is maintained for 1 hour and the mixture is allowed to warm to 20C over 18 hours. Then 50ml of water are added and a solution of HCl 1M is added to obtain an acidic aqueous phase. The solution is extracted with DCM. The crude product is purified by column chromatography (Eluant: 90/10 DCM/MeOH) to give 9.04g (yield=89%) of the title compound, Example 115, as a white solid. NMR 1H (DMSO d6) : delta 2.04 (s, 3H), 3.62-3.40 (m, 8H), 4.10-3.85 (m, 2H), 4.12 (d, 1H), 4.30 (d, 1H), 6.62 (t, 1HAr), 6.95 (d, 1HAr), 7.26 (d, 1HAr), 7.48 (t, 1HAr), 7.70 (m, 2HAr), 7.77 (s, 1HAr)., 13889-98-0

As the paragraph descriping shows that 13889-98-0 is playing an increasingly important role.

Reference：
Patent; CEPHALON, INC.; CEPHALON FRANCE; EP1586559; (2005); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.5747-48-8,11-(Piperazin-1-yl)dibenzo[b,f][1,4]thiazepine,as a common compound, the synthetic route is as follows.

Example 10 2-(2-(4-dibenzo[b,f][1,4]thiazepine-11-yl-1-piperazinyl)ethoxy)ethanol OR 11-[4-[2-(2-hydroxyethoxy)ethyl]-1-piperazinyl]dibenzo[b,f][1,4]thiazepine A 1 liter round bottom flask equipped with stirring rod, thermo pocket, water condenser was charged with solution of 11-piperazinyldibenzo[b,f][1,4]thiazepine in toluene 350 cc [63.0 g (0.22 moles)] and the mixture was stirred for 15 min 25-30 C., and, to which, was added sodium carbonate [41.0 gm (0.39 moles)], tetra butyl ammonium bromide [16.0 gm (0.05 moles)] and 2-(2-chloroethoxy)ethanol [32.0 gm (0.257 moles)] at room temperature. The reaction mixture was heated to reflux at 110-112 C. The reaction mixture was maintained at reflux for 10-12 hrs. The reaction mixture was analyzed by HPLC (to check absence of compound of formula IV) and was cooled to 25 C. to 30 C. To which, was added 150 cc DM water. Then the reaction mixture was stirred for 30 min at 25-30 C. The layers were separated and the aqueous layer extracted with 50 cc toluene. The extracts and the organic layer were combined, and the pH was adjusted to 2-3 using 1N HCl solution in DM (demineralized) water, the reaction mixture was then stirred for 30 min at 25-30 C. The layers were separated and the aqueous layer washed with 100 cc toluene twice. To the aqueous layer was added 250 cc toluene, and the pH was adjusted to 8-10 using sodium carbonate, the reaction mixture was stirred for 30 min at 25-30 C. The layers were separated and the aqueous layer extracted with 125 cc toluene. The extracts and the organic layer were combined, and washed with DM (demineralized) water 300 cc twice. The organic layer was distilled-off under vacuum below 70 C. to afford 2-(2-(4-dibenzo[b,f]-[1,4]thiazepine-11-yl-1-piperazinyl)ethoxy)ethanol Purity of 2-(2-(4-dibenzo[b,f]-[1,4]thiazepine-11-yl-1-piperazinyl)ethoxy)ethanol was 99.0 (area % by HPLC).

5747-48-8, The synthetic route of 5747-48-8 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Kansal, Vinod Kumar; Ahmad, Suhail; Lal, Kanhaiya; Patil, Bhatu Tumba; US2008/241949; (2008); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

120737-78-2, tert-Butyl 2-methylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 43A tert-butyl (2S)-4-[(6-{[5-(difluoromethyl)pyridin-2-yl]oxy}quinolin-2-yl)carbonyl]-2-methylpiperazine-1-carboxylate The product from Example 14A (200 mg, 0.632 mmol) was subjected to the conditions described in Example 14B, substituting (S)-tert-butyl 2-methylpiperazine-1-carboxylate for tert-butyl piperazine-1-carboxylate to give 155 mg (49%) of the titled compound., 120737-78-2

120737-78-2 tert-Butyl 2-methylpiperazine-1-carboxylate 15087784, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; AbbVie Inc.; Bogdan, Andrew; Cowart, Marlon D.; DeGoey, David A.; Jinkerson, Tammie K.; Koenig, John R.; Kort, Michael E.; Liu, Bo; Matulenko, Mark A.; Nelson, Derek W.; Patel, Meena V.; Peltier, Hillary; Scanio, Marc J.; Wakefield, Brian D.; US2015/218102; (2015); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.70261-82-4,4-(4-Methylpiperazin-1-ylmethyl)phenylamine,as a common compound, the synthetic route is as follows.

C the steps of the compound (50 mg, 0.16 mmol), 4 – ((4-methyl-piperazinyl) methyl) aniline (0.176 mmol), 1 – (3-dimethylamino-propyl) – 3-ethyl carbodiimide hydrochloride (0.24 mmol), 1-hydroxybenzotriazole and triazazole (0.24 mmol) and triethylamine (50 microliters) dissolved in dry N, N-dimethyl formamide in (3 ml), stir at room temperature overnight. Water 20 ml, ethyl acetate (10 ml, 5 times) extraction, extraction fluid after full and salt water washing, drying by anhydrous sodium sulfate, column chromatography (dichloromethane/methanol =1/10) separated to obtain title compound 20 mg per litre. MS:m/z, 499.2(M+H)., 70261-82-4

As the paragraph descriping shows that 70261-82-4 is playing an increasingly important role.

Reference：
Patent; CHIA TAI TIANQING PHARMACEUTICALGROUP CO LTD; Beijing Centaurus Biopharma Technology?Co.,?Ltd.; XIAO, DENGMING; LIANG, ZHI; HU, YUANDONG; HU, QUAN; ZHANG, QINGHUI; HAN, YONGXIN; WANG, HUAN; PENG, YONG; KONG, FANSHENG; LUO, HONG; (60 pag.)CN103130792; (2016); B;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

5308-25-8,5308-25-8, 1-Ethylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: A solution of compound 2 (0.55 mmol), 1-substituted piperazine (0.83 mmol) and pyridine (0.8 mmol) in 10 mL THF (tetrahydrofuran) was stirred at room temperature overnight. When the reaction was completed, the solvent was evaporated under reduced pressure. The residues were dissolved in ethyl acetate and washed with water and saturated sodium chloride solution. After drying over anhydrous Na2SO4, the solvent was removed under reduced pressure to get crude product. The pure products were obtained by recrystallizing from ethanol.

The synthetic route of 5308-25-8 has been constantly updated, and we look forward to future research findings.

Reference：
Article; Wu, Zhilin; Ding, Na; Tang, Yuting; Ye, Jiao; Peng, Junmei; Hu, Aixi; Research on Chemical Intermediates; vol. 43; 8; (2017); p. 4833 – 4850;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

262368-30-9, N-(4-Aminophenyl)-N-methyl-2-(4-methylpiperazin-1-yl)acetamide is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

10.5 [G] (30.0 [MMOL)] of [1-ACETYL-3- (1-ETHOXY-1-PHENYLMETHYLENE)-6-METHOXYCARBONYL-2-] indolinone (for preparation see WO 01/27081 mentioned above) and 8.60 g (33.0 [MMOL)] [N- [ (4-METHYL-PIPERAZIN-1-YL)-METHYLCARBONYL]-N-METHYL-P-PHENYLENEDIAMINE] (for preparation see WO 01/27081 mentioned above) are dissolved in 80 mL of dimethylformamide and stirred for 1 hour at [80C.] After cooling 6.50 mL of piperidine are added and the mixture is stirred for another two hours at ambient temperature. Water is added, the precipitate formed is suction filtered and washed with a little water. The residue is suspended in 200 mL of methanol, suction filtered and washed with cold water and diethyl ether. The substance is [DRIED IN VACUO] at 110 [C.] Yield : 12.4 g (77% of theory), [IR SPECTRUM] : 1610,1655, 1711 cm-1 Tm. p. = [253C] [EMPIRICAL FORMULA : C31H33N504] [ESI] mass spectrum: m/z = 540 [M+H]+ Elemental analysis: calculated: C 68.99 [H-6.] 16 [N 12.] 98 found: C 68.32 H 6.29 N 12.85, 262368-30-9

The synthetic route of 262368-30-9 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; BOEHRINGER INGELHEIM PHARMA GMBH & CO. KG; WO2004/13099; (2004); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

30459-17-7, 1-(4-Trifluoromethylphenyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,30459-17-7

Dark brown solid; IR (KBr, cm-1): v 3282 (-NH), 3068-3076 (-CH str.), 2223 (CN), 1256 (C-O-C), 833 (s-triazine C-N str.), 749 (C-F). 1H NMR (400 MHz, Me2SO-d6): delta 9.18 (s, 1H, -NH, s-triazine to amino-benzonitrile linkage), 8.10 (d, J = 7.4 Hz, 1H, C8 proton of quinoline), 7.77 (t, J = 7.6 Hz, 1H, C7 proton of quinoline), 7.59 (d, J = 8.6 Hz, 1H, C5 proton of quinoline), 7.52 (t, J = 7.2 Hz, 1H, C6 proton of quinoline), 7.39 (s, 1H, C3 proton of quinoline), 7.26-6.93 (7H, m, Ar-H), 3.89 (4H, br s, piperazine), 3.77 (s, 3H, N-CH3), 3.51 (4H, br s, piperazine). 13C NMR (100 MHz, Me2SO-d6): delta 175.8 (1C, C-6, s-triazine, C-N at piperazine linkage), 167.5 (1C, C-4, s-triazine, C-O-C at quinoline linkage), 165.5, 163.6 (2C, 1C at C-2, s-triazine, C-NH at benzonitrile moiety and 1C of CO), 144.8-116.7 (22C, Ar. C including 2C-CF3 at 129.9, 130.4 and 2CF3 at 125.2, 125.7), 105.9 (1C, CN), 95.8 (1C, -C-CN), 48.2, 45.6 (4C, piperazine ring carbon atoms), 30.6 (1C, N-CH3). 19F NMR (400 MHz, CDCl3): delta -66.03, -63.29 (6F, s, -CF3 of piperazine moiety and -CF3 of amino benzonitrile moiety).

30459-17-7 1-(4-Trifluoromethylphenyl)piperazine 121718, apiperazines compound, is more and more widely used in various fields.

Reference：
Article; Patel, Rahul V.; Kumari, Premlata; Rajani, Dhanji. P.; Chikhalia, Kishor H.; Journal of Fluorine Chemistry; vol. 132; 9; (2011); p. 617 – 627;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.655225-01-7,tert-Butyl 4-(2-bromoethyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

655225-01-7, STEP A: Sodium hydride (60percent mineral oil dispersion) (13.21 mg, 0.330 mmol) is added under nitrogen to the solution of (E)-2-amino-7-(4-fluoro-2-pyridin-3-yl-phenyl)-4-methyl-7,8-dihydro-6H- quinazolin-5-one oxime (Intermediate 1) (0.1 g, 0.275 mmol) in anhydrous DMF (4 mL). After 5 min, N-Boc-4-(2-bromoethyl)piperazine (161 mg, 0.550 mmol) is added and the mixture is heated at 50°C for 1.5 h. The suspension is diluted with H20 and extracted with EtOAc. The organic phase is dried over Na2S04, filtered and concentrated under reduced pressure. The beige-orange residue is purified by flash column chromatography (eluent DCM/MeOH from 99/1 to 95/5) to give the expected compound (0.111 g, 0.193 mmol, Yield: 70percent). LC-MS: method A, rt=1.60 min; (ES+), M+H+= 576.5 1H-NMR (DMSO-d6) delta (ppm): 8.57 (dd, J=4.84, 1.61 Hz, 1 H); 8.53 (dd, J=2.2Q, 0.73 Hz, 1 H): 7.76 (ddd, J=7.92, 2.35, 1.76 Hz, 1 H); 7.66 (dd, J=8.80, 5.87 Hz, 1 H); 7.45 (ddd, J=7.78, 4.84, 0.88 Hz, 1 H); 7.31 (td, J=8.73, 2.79 Hz, 1 H); 7.1 1 (dd, J=9.68, 2.93 Hz, 1 H); 6.76 (s, 2 H); 4.15 (t, J=5.87 Hz, 2 H); 3.24-3.28 (m, 4 H); 2.94-3.08 (m, 2 H); 2.82-2.94 (m, 1 H); 2.54-2.66 (m, 4 H); 2.45 (s, 3 H); 2.32-2.39 (m, 4 H); 1.39 (s, 9 H)

As the paragraph descriping shows that 655225-01-7 is playing an increasingly important role.

Reference：
Patent; DAC SRL; AMICI, Raffaella; COLOMBO, Andrea; COURTNEY, Stephen Martin; MERCURIO, Ciro; MONTALBETTI, Christian Aldo Georges Napoleon; MORTONI, Annalisa; VARASI, Mario; WO2013/64919; (2013); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics